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US 5,204,465 AGranted
Process for the production of piperazinylpyrimidine derivatives
AssigneeLonza Ltd.
InventorsDavid L. Kuo, Robert Voeffray
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Abstract
A process for the production of piperazinylpyrimidine derivatives of the formula: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are the same or different and each is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group, branched or unbranched. These piperazinylpyrimidine derivatives are acid-converted with cyanamide to an amidine salt starting from piperazine or its hydrate and then reacted with a dicarbonyl compound in the presence of a base to the end product.
Claims19
Process for the production of a piperazinylpyrimidine compound of the formula:
- ##STR8## wherein R.sub.1, R.sub.2 and R.sub.3 are the same or different and each is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group, branched or unbranched, characterized in that, in a first stage, piperazine of the formula:
- ##STR9## or its hydrate is acid-reacted with cyanamide to an amidine salt of the formula:
- ##STR10## wherein X is an anion which forms said amidine salt and n corresponds to the valence of said anion which forms said amidine salt, the amidine salt of formula III is optionally isolated, and then, in a second stage, the amidine salt of formula III is reacted with a CH-acidic compound to said piperazinylpyrimidine compound of formula I.
Dependencies are inferred from the claim text.